[CAS NO. 447410-57-3]  SB756050

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PRODUCTS SPECIFICATIONS [447410-57-3]

Catalog
HY-102016
Brand
MCE
CAS
447410-57-3

DESCRIPTION [447410-57-3]

Overview

MDLMFCD02585318
Molecular Weight500.59
Molecular FormulaC21H28N2O8S2
SMILESO=S(N1CCN(S(=O)(C2=CC=C(OC)C(OC)=C2)=O)CCC1)(C3=CC=C(OC)C(OC)=C3)=O

For research use only. We do not sell to patients.


Summary

SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.


In Vitro

TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D) [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different [1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00733577 GlaxoSmithKline
Diabetes Mellitus, Type 2
August 11, 2008 Phase 1
NCT00607906 GlaxoSmithKline
Diabetes Mellitus, Type 2
November 16, 2007 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 150 mg/mL ( 299.65 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9976 mL 9.9882 mL 19.9764 mL
5 mM 0.3995 mL 1.9976 mL 3.9953 mL
10 mM 0.1998 mL 0.9988 mL 1.9976 mL
* Please refer to the solubility information to select the appropriate solvent.